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Submit ReviewTalabostat mesylate
Description: Potent DPP IV inhibitor; activates NLRP1b inflammasome
Alternative Names: Val-boroPro,BXCL 701
Chemical Name: B-[(2R)-1-[(2S)-2-Amino-3-methyl-1-oxobutyl]-2-pyrrolidinyl]boronic acid methanesulfonate
Purity: ≥98% (HPLC)
Biological Activity for Talabostat mesylate
Talabostat mesylate is a potent DPP IV inhibitor (IC50 values are <4, 4, 11, 310 and 560 nM at DPP4, DPP8, DPP9, DPP7 and FAP, respectively). Activates the inflammasome sensor protein NLRP1b and selectively triggers pyroptosis in monocytes and macrophages. Induces immune-mediated tumor regression in multiple mouse models of cancer. Orally bioavailable.
Technical Data for Talabostat mesylate
| M. Wt | 310.18 |
| Formula | C9H19BN2O3.CH3SO3H |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 150080-09-4 |
| PubChem ID | 11522448 |
| InChI Key | OXYYOEIGQRXGPI-WSZWBAFRSA-N |
| Smiles | O=C([C@@H](N)C(C)C)N1CCC[C@H]1B(O)O.CS(O)(=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Talabostat mesylate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 31.02 | 100 | |
| DMSO | 15.51 | 50 |
Preparing Stock Solutions for Talabostat mesylate
The following data is based on the product molecular weight 310.18. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 3.22 mL | 16.12 mL | 32.24 mL |
| 5 mM | 0.64 mL | 3.22 mL | 6.45 mL |
| 10 mM | 0.32 mL | 1.61 mL | 3.22 mL |
| 50 mM | 0.06 mL | 0.32 mL | 0.64 mL |
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Product Datasheets for Talabostat mesylate
References for Talabostat mesylate
References are publications that support the biological activity of the product.
Okondo et al (2017) DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat.Chem.Biol. 13 46 PMID: 27820798
Okondo et al (2018) Inhibition of Dpp8/9 activates the Nlrp1b inflammasome. Cell Chem.Biol. 25 262 PMID: 29396289
If you know of a relevant reference for Talabostat mesylate, please let us know.
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Keywords: Talabostat mesylate, Talabostat mesylate supplier, Potent, DPP, IV, inhibitors, inhibits, inflammasome, pyroptosis, Nlrp1b, BXCL701, DPP4, Val-boroPro, BXCL, 701, Dipeptidyl, Peptidase, (DPP-IV), Inflammasomes, 3719, Tocris Bioscience
5 Citations for Talabostat mesylate
Citations are publications that use Tocris products. Selected citations for Talabostat mesylate include:
Massimiliano et al (2022) PhAc-ALGP-Dox, a Novel Anticancer Prodrug with Targeted Activation and Improved Therapeutic Index. Mol Cancer Ther 21 568-581 PMID: 35149549
Daniel A et al (2022) A ubiquitin-independent proteasome pathway controls activation of the CARD8 inflammasome. J Biol Chem 298 102032 PMID: 35580636
Justin R et al (2022) M24B aminopeptidase inhibitors selectively activate the CARD8 inflammasome. Nat Chem Biol 18 565-574 PMID: 35165443
Orth-He et al (2023) Protein folding stress potentiates NLRP1 and CARD8 inflammasome activation. Cell Rep 42 111965 PMID: 36649711
Henrik et al (2020) The half-life of the bone-derived hormone osteocalcin is regulated through O-glycosylation in mice, but not in humans. Elife 9 PMID: 33284103
Do you know of a great paper that uses Talabostat mesylate from Tocris? Please let us know.
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